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P2Y 12-receptor antagonist - Novel antagonists of the P2Y12-receptor with antithrombotic effect

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05.03.2008

Purinergic receptors have been in the focus of drug discovery for many years. Modulation of P2 receptors in platelets is of paramount importance in regulating platelet function, and, as a consequence, in controlling thrombotic diseases, which are the most common cause of morbidity and mortality in the Western world. The P2Y12-receptor on blood platelets is the target of known antithrombotic drugs (e.g. clopidogrel). The receptor is therefore validated for this therapeutic use. Furthermore, the P2Y12-receptor is expressed in certain parts of the brain, which opens new routes for the treatment of neuroinflammatory and neurodegenerative diseases. This invention provides novel antagonists of the P2Y12- receptor. The disclosed novel compounds show reversible and selective binding to the P2Y12-receptor. The molecules do not require bioactivation. Further the patent application discloses synthesis of the compounds with optimised product yield.

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